COX

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1261	Celecoxib	<1 mg/mL	76 mg/mL	33 mg/mL
S1255	Nepafenac	<1 mg/mL	50 mg/mL	<1 mg/mL
S1638	Ibuprofen	<1 mg/mL	41 mg/mL	41 mg/mL
S1723	Indomethacin	<1 mg/mL	72 mg/mL	24 mg/mL
S2007	Sulindac	<1 mg/mL	71 mg/mL	9 mg/mL
S5418	Parecoxib Sodium	-1 mg/mL	78 mg/mL	-1 mg/mL
S5010	Indometacin Sodium	-1 mg/mL	87 mg/mL	-1 mg/mL
S5711	Deracoxib	<1 mg/mL	80 mg/mL	20 mg/mL
S5520	Phenidone	-1 mg/mL	32 mg/mL	-1 mg/mL
S3043	Rofecoxib	<1 mg/mL	63 mg/mL	<1 mg/mL
S1734	Meloxicam	<1 mg/mL	30 mg/mL	<1 mg/mL
S4028	Dexamethasone Sodium Phosphate	103 mg/mL	<1 mg/mL	<1 mg/mL
S3023	Bufexamac	<1 mg/mL	45 mg/mL	3 mg/mL
S3017	Aspirin	<1 mg/mL	36 mg/mL	36 mg/mL
S1761	Suprofen	<1 mg/mL	52 mg/mL	52 mg/mL
S1713	Piroxicam	<1 mg/mL	66 mg/mL	1 mg/mL
S1328	Etodolac	<1 mg/mL	58 mg/mL	58 mg/mL
S1645	Ketoprofen	<1 mg/mL	51 mg/mL	51 mg/mL
S1903	Diclofenac Sodium	14 mg/mL	64 mg/mL	64 mg/mL
S1518	Ibuprofen Lysine	71 mg/mL	<1 mg/mL	<1 mg/mL
S2047	Lornoxicam	<1 mg/mL	3 mg/mL	<1 mg/mL
S1646	Ketorolac	<1 mg/mL	75 mg/mL	75 mg/mL
S1626	Naproxen Sodium	50 mg/mL	3 mg/mL	<1 mg/mL
S2903	Lumiracoxib	<1 mg/mL	59 mg/mL	<1 mg/mL
S2531	Asaraldehyde	<1 mg/mL	39 mg/mL	16 mg/mL
S1960	Pranoprofen	<1 mg/mL	51 mg/mL	6 mg/mL
S3008	Zaltoprofen	<1 mg/mL	60 mg/mL	31 mg/mL
S2602	Acemetacin	<1 mg/mL	83 mg/mL	58 mg/mL
S1959	Tolfenamic Acid	<1 mg/mL	52 mg/mL	<1 mg/mL
S4049	Valdecoxib	<1 mg/mL	63 mg/mL	18 mg/mL
S2577	Phenacetin	<1 mg/mL	36 mg/mL	36 mg/mL
S2040	Nimesulide	<1 mg/mL	62 mg/mL	<1 mg/mL
S4149	Amfenac Sodium Monohydrate	59 mg/mL	59 mg/mL	4 mg/mL
S4248	Bromfenac Sodium	71 mg/mL	71 mg/mL	2 mg/mL
S4051	Nabumetone	<1 mg/mL	46 mg/mL	25 mg/mL
S3018	Niflumic acid	<1 mg/mL	56 mg/mL	<1 mg/mL
S3173	Antipyrine	38 mg/mL	38 mg/mL	38 mg/mL
S4011	Ampiroxicam	<1 mg/mL	90 mg/mL	<1 mg/mL
S8433	NS-398 (NS398)	<1 mg/mL	62 mg/mL	<1 mg/mL
S4032	Bismuth Subsalicylate	<1 mg/mL	0.04 mg/mL	<1 mg/mL
S4628	(+/-)-Sulfinpyrazone	<1 mg/mL	80 mg/mL	64 mg/mL
S4136	Carprofen	<1 mg/mL	55 mg/mL	55 mg/mL
S3063	Diclofenac Diethylamine	<1 mg/mL	74 mg/mL	74 mg/mL
S4656	Parecoxib	<1 mg/mL	74 mg/mL	2 mg/mL
S4609	Diflunisal	<1 mg/mL	50 mg/mL	20 mg/mL
S4176	Trometamol	24 mg/mL	2 mg/mL	<1 mg/mL
S4078	Mefenamic Acid	<1 mg/mL	48 mg/mL	<1 mg/mL
S4651	Etoricoxib	<1 mg/mL	71 mg/mL	46 mg/mL
S4230	Oxaprozin	<1 mg/mL	59 mg/mL	27 mg/mL
S2349	Rutaecarpine	<1 mg/mL	24 mg/mL	<1 mg/mL
S2351	Salicin	24 mg/mL	57 mg/mL	<1 mg/mL
S4526	Fenbufen	<1 mg/mL	50 mg/mL	50 mg/mL
S4539	Salicylic acid	<1 mg/mL	27 mg/mL	27 mg/mL
S7889	Xanthohumol	<1 mg/mL	70 mg/mL	70 mg/mL
S2108	Flunixin Meglumin	98 mg/mL	98 mg/mL	8 mg/mL
S4295	Meclofenamate Sodium	63 mg/mL	63 mg/mL	63 mg/mL

特异性亚型抑制剂

COX抑制剂（57）
新COX产品

产品目录	产品描述	文献引用	实验数据
S1261	Celecoxib Celecoxib是一种选择性COX-2抑制剂，在Sf9细胞中IC50为40 nM。	Sci Transl Med, 2018, 10(433) Blood, 2011, 118(22):5891-900 Br J Pharmacol, 2014, 171(2):498-508	Tumors were resected from mice 10 days after orthotopic inoculation of 4T1-Luc2 cells, and hydrogels loaded with the following payloads were evaluated: anti–PD-1, anti-CTLA-4, IL-15sa, lenalidomide, celecoxib, STING-RR, or R848. Mice that did not receive a hydrogel were examined as a negative control. (A) IVIS imaging of 4T1-Luc2 cells is shown for all groups described and illustrates tumor burden.
S1255	Nepafenac Nepafenac是一种非甾体抗炎药剂。
S1638	Ibuprofen Ibuprofen 是一种抗炎类抑制剂，作用于COX-1和COX-2，IC50分别为13 μM和370 μM。
S1723	Indomethacin Indomethacin是一种非选择性的COX1和COX2的抑制剂，IC50分别为0.1 μg/mL和5 μg/mL。常用于降低发热、减缓疼痛、僵硬和肿胀。	Nat Commun, 2016, 7:12885 Theranostics, 2017, 7(5):1389-1406	Indicated PN and MES spheres were shown expressing GFP under the control of a 7 × TCF/LEF optimal promoter cassette (7 × TOP) and constitutively expressed nuclear mCherry. PN 84 and MES 1123 were treated with Wnt3a (200 ng/ml), indomethacin (Indo; 20 μM), or a control (vehicle). Scale bar, 100 μm. Bar graph, quantification of fluorescent signal of GFP (TOP-GFP) versus mCherry (PGK-H2BmCherry). The percentage of GFP- and mCherry-positive spheres was determined by FACS.
S2007	Sulindac Sulindac 是一种非甾体类的COX抑制剂，有效地抑制了前列腺素的合成，用来治疗急性或者慢性炎症。	Oncogene, 2017, 36(6):787-796 Oncogene, 2016, 10.1038/onc.2016.247	(d) Parental and regorafenib-resistant HCT116 cells were treated with 40 μM regorafenib, 20 μM sorafenib, 1 μM UCN-01, 1 μM YM-155, 10 μM roscovitine, 15 μM sunitinib, 10 μM crizotinib, 10 nM TRAIL, 10 μM VX680, 20 μM etoposide, 20 μM temsirolimus or 120 μM sulindac sulfide for 48 h. Apoptosis was analyzed as in b. (e) Western blotting of Mcl-1 in parental and regorafenib-resistant HCT116 cells treated with indicated agents as in d for 24 h. Results in (b-d) represent the means±s.d. of three independent experiments. NS, P>0.05; P<0.05; *P<0.01.
S5418^New	Parecoxib Sodium Parecoxib Sodium is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2).
S5010^New	Indometacin Sodium Indomethacin Sodium is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects.
S5711^New	Deracoxib Deracoxib is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3).
S5520^New	Phenidone Phenidone, a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer.
S3043	Rofecoxib Rofecoxib 是一种COX-2抑制剂，IC50为18 nM。	Toxicol Appl Pharmacol, 2015, 285(1):51-60
S1734	Meloxicam Meloxicam 是一种选择性的COX抑制剂，用于缓解疼痛以及发烧症状。	Oncol Lett, 2017, 14(2):2198-2206	Meloxicam (0.25 μg/ml) decreases the migration of CF41.Mg cells. Incubation with 0.25 μg/ml meloxicam for 24 and 48 h inhibited the migration of cells compared with the DMSO‑treated control cells in a wound healing assay. A total of 6 repeats were performed and results are presented as the mean ± standard deviation. Representative images of the wound healing assay and quantification if the results are presented. Scale bar, 90 μm. *P<0.05 vs. the control group.
S4028	Dexamethasone Sodium Phosphate Dexamethasone Sodium Phosphate是一种白介素受体抑制剂，抑制COX-2。		Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S3023	Bufexamac Bufexamac是一种COX抑制剂，靶点是IFN-α， EC50 为8.9 μM。	Nat Biotechnol, 2015, 10.1038/nbt.3130 Oncotarget, 2016, 7(37):59388-59401	(a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm.
S3017	Aspirin Aspirin是水杨酸类不可逆的COX1 and COX2抑制剂，常用作止痛药来缓解轻微疼痛，作为解热药减少发热，并作为一种抗炎药物。	Toxicol Appl Pharmacol, 2015, 285(1):51-60
S1761	Suprofen Suprofen 是一种双重的COX-1/COX-2抑制剂，用作抗炎症的镇痛剂或者退热剂。
S1713	Piroxicam Piroxicam 是一种非选择性COX抑制剂，IC50为6 mM。
S1328	Etodolac Etodolac 是COX抑制剂，IC50为53.5 nM。
S1645	Ketoprofen Ketoprofen 是双重 COX1/2 抑制剂，是非选择性的NSAID，作用于人重组COX-1和COX-2的 IC50分别为0.5 μM和2.33 μM。
S1903	Diclofenac Sodium Diclofenac Sodium是非选择性COX抑制剂，作用于绵羊COX-1和COX-2， IC50分别为60和220 nM。	Cell, 2016, 167(7):1803-1813 Head Neck, 2014, 10.1002/hed.23822
S1518	Ibuprofen Lysine Ibuprofen Lysine 是一种非甾体类抗炎药。
S2047	Lornoxicam Lornoxicam是COX-1和COX-2抑制剂，IC50分别为5 nM和8 nM。
S1646	Ketorolac Ketorolac是一种非选择性的COX抑制剂，作用于人类COX-1和COX-2时， IC50分别为1.23 µM和3.50 µM。
S1626	Naproxen Sodium Naproxen Sodium 是一种非选择性环氧合酶(COX)抑制剂，作用于COX-1和COX-2时，IC50分别为8.7 μM和5.2 μM。
S2903	Lumiracoxib Lumiracoxib是一种新型，选择性的COX-2抑制剂，K_i为0.06 μM；对COX1的K_i值为3 μM。	Biochem Pharmacol, 2017, 135:139-150 Xenobiotica, 2016, 10.1080/00498254.2016.1206239	Blood concentration-time profiles for lumiracoxib following single oral administration at 10 mg/kg to (a) Hu-FRGTM mice (n = 3) and (b) to Mu-FRGTM mice (n = 3). Symbols represent concentration-time profiles from individual animals.
S2531	Asaraldehyde Asaraldehyde是一种天然的COX-2抑制剂，比作用于COX-1选择性高17倍。
S1960	Pranoprofen Pranoprofen是PGE2抑制剂，IC50为7.5 μM。
S3008	Zaltoprofen Zaltoprofen是COX-1和COX-2抑制剂,用于治疗关节炎。
S2602	Acemetacin Acemetacin是一种非甾体类抗炎药，是吲哚美辛的乙醇酸酯，是一种环加氧酶抑制剂。
S1959	Tolfenamic Acid Tolfenamic Acid是一种COX-2抑制剂，IC50为0.2 μM。
S4049	Valdecoxib Valdecoxib是一种强有效和选择性的COX-2抑制剂，IC50为5nM.	Biochem Bioph Res Co, 2015, 460(2):198-204	(B) HeLa and SACC-83 cells were treated with radiation, valdecoxib, or both radiation and valdecoxib. Cells were lysed or extracted for membrane proteins and then subjected to Western blot.
S2577	Phenacetin Phenacetin是一种非阿片类镇痛剂，没有抗炎特性。
S2040	Nimesulide Nimesulide是一种选择性COX-2抑制剂，IC50为26 μM。	Viruses, 2015, 7(5):2268-87	Nimesulide has no effect on KSHV lytic replication in BCBL-1 cells. The cells induced with TPA for 3 h were treated with the test compounds for 72 h. Then, the effect of nimesulide on cell viability (C) and the number of DNA copies (D) were measured as described in the Methods. CDV (20 µM) is a positive control for inhibiting viral DNA replication. Data were normalized as the fold change compared with the no-TPA induced control. The results are presented as the mean values with standard deviations (n = 3).
S4149	Amfenac Sodium Monohydrate Amfenac Sodium Monohydrate是一种非甾体类镇痛消炎药。对COX1和COX2的IC50分别为250 nM和150 nM。
S4248	Bromfenac Sodium Bromfenac Sodium是一种非甾体类抗炎药(NSAID)，具有抗炎活性，通过抑制环氧合酶1和2可阻断前列腺素的合成。
S4051	Nabumetone Nabumetone是一种非甾类抗炎症药物，它的活性代谢物抑制COX。
S3018	Niflumic acid Niflumic acid是环氧合酶-2 (COX-2)抑制剂,用于治疗关节和肌肉疼痛。
S3173	Antipyrine Antipyrine 是一种镇痛剂和退热剂，选择性COX3抑制剂。
S4011	Ampiroxicam Ampiroxicam是一种非选择性的cyclooxygenase（环氧合酶）抑制剂，作为消炎药。
S8433	NS-398 (NS398) NS-398是一种选择性的COX-2抑制剂，对人源重组的COX-1和COX-2的IC50分别为75 μM和1.77μM。		(C)Percentage of TUNEL-positive cell in B were calculated. Data are mean ± SEM; ** P < 0.01 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (D-G) ELISA of cytokines IL-1α (D), IL-1β (E), IL-6 (F), and TNF-α (G) in tSCI rats with or without NS-398 treatment. Data are mean ± SEM; * P < 0.05 or P < 0.01 versus the Sham group; # P <0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (H) The mean CBS score in tSCI rats was improved by NS-398 treatment. Data are mean ± SEM; P < 0.05 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group.
S4032	Bismuth Subsalicylate Bismuth Subsalicylate 是Pepto-Bismol的有效成分，可以抑制前列腺素G/H合成酶1/2。
S4628	(+/-)-Sulfinpyrazone Sulfinpyrazone是研究得最多的血小板COX抑制剂之一，还是一种能在肾脏近端小管中，竞争性抑制尿酸重吸收的尿酸排泄剂。
S4136	Carprofen Carprofen 抑制犬科COX2，IC50为30 nM。
S3063	Diclofenac Diethylamine Diclofenac Diethylamine是一种非类固醇消炎药，用于减轻炎症和某些状况下的止痛药。Diclofenac通过抑制COX1和COX2来抑制前列腺素合成，发挥其功能。
S4656	Parecoxib Parecoxib是选择性COX2的抑制剂。
S4609	Diflunisal Diflunisal是水杨酸的二氟苯基衍生物，是非类固醇的消炎药。具有退热、止痛和消炎特性。它是环氧酶抑制剂。
S4176	Trometamol Trometamol是一种质子受体，用于治疗酸血症。它能抑制COX1和COX2，因而抑制花生四烯酸向炎性前列腺素的转变。
S4078	Mefenamic Acid Mefenamic Acid是一种竞争性COX-1和COX-2抑制剂。
S4651	Etoricoxib Etoricoxib是一种新型的COX-2选择性抑制剂，具有抗炎、退热、止痛和潜在的抗肿瘤活性。
S4686	Vitamin E Vitamin E是一种脂溶性的维生素，具有有效的抗氧化特性。它是有效的过氧化氢自由基清除剂并在很多组织中，非竞争性地抑制环氧酶活性。同时通过抑制VEGF基因转录，抑制血管生成和肿瘤休眠。
S4230	Oxaprozin Oxaprozin 是一种非麻醉性，非甾体类抗炎药（NSAID），用于缓解与骨关节炎和类风湿关节炎相关的炎症，肿胀，僵硬，关节疼痛。
S2349	Rutaecarpine Rutaecarpine是从 Evodia rutaecarpa和相关草药中分离的indolopyridoquinazolinone生物碱。是一种新型的COX2抑制剂。
S2351	Salicin Salicin是一种醇-β-糖苷，含有D-葡萄糖。是柳树皮产生的一种抗炎剂。它是一种天然的、非选择性的COX1和COX2抑制剂。
S4526	Fenbufen Fenbufen是一种具有口服活性的苯基链烷衍生物（phenylalkanoic derivative），它具有抗炎、止痛、解热的活性，是一种非固醇类的消炎药。
S4539	Salicylic acid Salicylic acid是一种水杨酸，植物中的天然化合物，是乙烯生物合成和环氧酶活性的抑制剂。
S7889	Xanthohumol Xanthohumol，来自啤酒花的一种异戊烯化查耳酮，抑制COX-1和COX-2活性，并表现出化学预防作用。Phase 1。
S2108	Flunixin Meglumin Flunixin Meglumin是一种有效的环氧化酶抑制剂，用作镇痛剂，具有抗炎和退热的活性。
S4295	Meclofenamate Sodium Meclofenamate Sodium是一种双COX-1/COX-2抑制剂，其IC50 分别为40 nM 和 50 nM，用于治疗关节、肌肉疼痛，关节炎以及痛经。

研究领域

产品类型

COX

信号通路图

研究领域

特异性亚型抑制剂